Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based β-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01917
Abstract: Accumulation of amyloid β peptides (Aβ) is thought to be one of the causal factors of Alzheimer's disease (AD). The aspartyl protease β-site amyloid precursor protein cleaving enzyme 1 (BACE1) is the rate-limiting protease for… read more here.
Keywords: trial; protein cleaving; precursor protein; cleaving enzyme ... See more keywords
Discovery of an Extremely Potent Thiazine-Based β-Secretase (BACE1) Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b01140
Abstract: Genetic evidence points to deposition of amyloid-β (Aβ) as a causal factor for Alzheimer's disease. Aβ generation is ini-tiated when β-secretase (BACE1) cleaves the amyloid precursor protein. Starting with an oxazine lead 1, we describe… read more here.
Keywords: bace1 inhibitor; thiazine based; low projected; secretase bace1 ... See more keywords